JP2008521831A5 - - Google Patents
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- Publication number
- JP2008521831A5 JP2008521831A5 JP2007543613A JP2007543613A JP2008521831A5 JP 2008521831 A5 JP2008521831 A5 JP 2008521831A5 JP 2007543613 A JP2007543613 A JP 2007543613A JP 2007543613 A JP2007543613 A JP 2007543613A JP 2008521831 A5 JP2008521831 A5 JP 2008521831A5
- Authority
- JP
- Japan
- Prior art keywords
- optionally substituted
- optionally
- substituted lower
- heterocycloalkyl
- group
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Pending
Links
- 125000003342 alkenyl group Chemical group 0.000 claims 28
- 125000000304 alkynyl group Chemical group 0.000 claims 28
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 24
- 229910052799 carbon Inorganic materials 0.000 claims 24
- 125000001072 heteroaryl group Chemical group 0.000 claims 22
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 22
- 125000000217 alkyl group Chemical group 0.000 claims 21
- 125000001316 cycloalkyl alkyl group Chemical group 0.000 claims 18
- 125000004475 heteroaralkyl group Chemical group 0.000 claims 18
- 125000005885 heterocycloalkylalkyl group Chemical group 0.000 claims 18
- 229910052739 hydrogen Inorganic materials 0.000 claims 18
- 239000001257 hydrogen Substances 0.000 claims 18
- 150000002431 hydrogen Chemical class 0.000 claims 18
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 18
- 125000003710 aryl alkyl group Chemical group 0.000 claims 16
- 229910052757 nitrogen Inorganic materials 0.000 claims 14
- IJGRMHOSHXDMSA-UHFFFAOYSA-N nitrogen Substances N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 14
- 125000003107 substituted aryl group Chemical group 0.000 claims 14
- 150000001336 alkenes Chemical class 0.000 claims 12
- 150000001345 alkine derivatives Chemical class 0.000 claims 12
- 150000001875 compounds Chemical class 0.000 claims 12
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 10
- 229910052760 oxygen Inorganic materials 0.000 claims 10
- 125000001153 fluoro group Chemical group F* 0.000 claims 9
- QVGXLLKOCUKJST-UHFFFAOYSA-N atomic oxygen Chemical group [O] QVGXLLKOCUKJST-UHFFFAOYSA-N 0.000 claims 8
- 239000001301 oxygen Substances 0.000 claims 8
- 125000005843 halogen group Chemical group 0.000 claims 6
- 229910052717 sulfur Inorganic materials 0.000 claims 6
- 201000010099 disease Diseases 0.000 claims 5
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical group [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims 4
- 239000011593 sulfur Substances 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 3
- 125000004414 alkyl thio group Chemical group 0.000 claims 3
- 239000000203 mixture Substances 0.000 claims 3
- 208000000103 Anorexia Nervosa Diseases 0.000 claims 2
- 208000032928 Dyslipidaemia Diseases 0.000 claims 2
- 206010019280 Heart failures Diseases 0.000 claims 2
- 208000017170 Lipid metabolism disease Diseases 0.000 claims 2
- 208000008589 Obesity Diseases 0.000 claims 2
- 102000003728 Peroxisome Proliferator-Activated Receptors Human genes 0.000 claims 2
- 108090000029 Peroxisome Proliferator-Activated Receptors Proteins 0.000 claims 2
- 206010067584 Type 1 diabetes mellitus Diseases 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 2
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 2
- 235000020824 obesity Nutrition 0.000 claims 2
- 239000000651 prodrug Substances 0.000 claims 2
- 229940002612 prodrug Drugs 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 208000011580 syndromic disease Diseases 0.000 claims 2
- 208000024827 Alzheimer disease Diseases 0.000 claims 1
- 206010003210 Arteriosclerosis Diseases 0.000 claims 1
- 201000001320 Atherosclerosis Diseases 0.000 claims 1
- 208000023328 Basedow disease Diseases 0.000 claims 1
- 206010007559 Cardiac failure congestive Diseases 0.000 claims 1
- 208000024172 Cardiovascular disease Diseases 0.000 claims 1
- 206010007749 Cataract diabetic Diseases 0.000 claims 1
- 108700012841 Cholesteryl Ester Transfer Protein Deficiency Proteins 0.000 claims 1
- 208000006545 Chronic Obstructive Pulmonary Disease Diseases 0.000 claims 1
- 208000011231 Crohn disease Diseases 0.000 claims 1
- 201000004624 Dermatitis Diseases 0.000 claims 1
- 208000002249 Diabetes Complications Diseases 0.000 claims 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 claims 1
- 206010012655 Diabetic complications Diseases 0.000 claims 1
- 206010012689 Diabetic retinopathy Diseases 0.000 claims 1
- 206010017943 Gastrointestinal conditions Diseases 0.000 claims 1
- 208000002705 Glucose Intolerance Diseases 0.000 claims 1
- 208000015023 Graves' disease Diseases 0.000 claims 1
- 208000001204 Hashimoto Disease Diseases 0.000 claims 1
- 208000030836 Hashimoto thyroiditis Diseases 0.000 claims 1
- 208000035150 Hypercholesterolemia Diseases 0.000 claims 1
- 206010060378 Hyperinsulinaemia Diseases 0.000 claims 1
- 208000031226 Hyperlipidaemia Diseases 0.000 claims 1
- 206010020772 Hypertension Diseases 0.000 claims 1
- 206010061218 Inflammation Diseases 0.000 claims 1
- 206010022489 Insulin Resistance Diseases 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 206010033307 Overweight Diseases 0.000 claims 1
- 208000002193 Pain Diseases 0.000 claims 1
- 208000018737 Parkinson disease Diseases 0.000 claims 1
- 241000721454 Pemphigus Species 0.000 claims 1
- 201000004681 Psoriasis Diseases 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- 208000021386 Sjogren Syndrome Diseases 0.000 claims 1
- 208000007536 Thrombosis Diseases 0.000 claims 1
- 206010046851 Uveitis Diseases 0.000 claims 1
- 206010047642 Vitiligo Diseases 0.000 claims 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 claims 1
- 208000022531 anorexia Diseases 0.000 claims 1
- 230000036528 appetite Effects 0.000 claims 1
- 235000019789 appetite Nutrition 0.000 claims 1
- 208000011775 arteriosclerosis disease Diseases 0.000 claims 1
- 208000006673 asthma Diseases 0.000 claims 1
- 208000010668 atopic eczema Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 208000017760 chronic graft versus host disease Diseases 0.000 claims 1
- 208000029078 coronary artery disease Diseases 0.000 claims 1
- 206010061428 decreased appetite Diseases 0.000 claims 1
- 201000001981 dermatomyositis Diseases 0.000 claims 1
- 206010012601 diabetes mellitus Diseases 0.000 claims 1
- 201000007025 diabetic cataract Diseases 0.000 claims 1
- 208000033679 diabetic kidney disease Diseases 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000037406 food intake Effects 0.000 claims 1
- 235000012631 food intake Nutrition 0.000 claims 1
- 208000015076 hyperalphalipoproteinemia Diseases 0.000 claims 1
- 230000003451 hyperinsulinaemic effect Effects 0.000 claims 1
- 201000008980 hyperinsulinism Diseases 0.000 claims 1
- 208000006575 hypertriglyceridemia Diseases 0.000 claims 1
- 201000008319 inclusion body myositis Diseases 0.000 claims 1
- 208000000509 infertility Diseases 0.000 claims 1
- 230000036512 infertility Effects 0.000 claims 1
- 231100000535 infertility Toxicity 0.000 claims 1
- 230000002757 inflammatory effect Effects 0.000 claims 1
- 230000004054 inflammatory process Effects 0.000 claims 1
- 208000002780 macular degeneration Diseases 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 201000006417 multiple sclerosis Diseases 0.000 claims 1
- 230000004770 neurodegeneration Effects 0.000 claims 1
- 208000015122 neurodegenerative disease Diseases 0.000 claims 1
- 230000002981 neuropathic effect Effects 0.000 claims 1
- 230000036407 pain Effects 0.000 claims 1
- 208000005987 polymyositis Diseases 0.000 claims 1
- 201000009104 prediabetes syndrome Diseases 0.000 claims 1
- 230000002685 pulmonary effect Effects 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 208000001072 type 2 diabetes mellitus Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US63189304P | 2004-11-30 | 2004-11-30 | |
| US71525805P | 2005-09-07 | 2005-09-07 | |
| PCT/US2005/043412 WO2006060535A2 (en) | 2004-11-30 | 2005-11-29 | Indole derivatives for use as ppar active compounds |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2008521831A JP2008521831A (ja) | 2008-06-26 |
| JP2008521831A5 true JP2008521831A5 (enExample) | 2009-01-22 |
Family
ID=36284449
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2007543613A Pending JP2008521831A (ja) | 2004-11-30 | 2005-11-29 | Ｐｐａｒ活性化合物 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US20060135540A1 (enExample) |
| EP (1) | EP1833787A2 (enExample) |
| JP (1) | JP2008521831A (enExample) |
| AU (1) | AU2005311826A1 (enExample) |
| CA (1) | CA2589896A1 (enExample) |
| WO (1) | WO2006060535A2 (enExample) |
Families Citing this family (52)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7629473B2 (en) * | 2005-06-17 | 2009-12-08 | H. Lundbeck A/S | 2-(1H-indolylsulfanyl)-aryl amine derivatives |
| AR054393A1 (es) * | 2005-06-17 | 2007-06-20 | Lundbeck & Co As H | Derivados de benzo(b)furano y benzo(b)tiofeno, composiciones farmaceuticas que los contienen y su uso en la fabricacion de un medicamento para el tratamiento de enfermedades mediadas por la inhibicion de la reabsorcion de neurotransmisores de amina biogenicos. |
| FR2890071B1 (fr) | 2005-08-30 | 2007-11-09 | Fournier Sa Sa Lab | Nouveaux composes de l'indole |
| US20070249561A1 (en) * | 2006-04-25 | 2007-10-25 | Taylor Bradley K | Pharmacological method for treatment of neuropathic pain |
| WO2008063888A2 (en) | 2006-11-22 | 2008-05-29 | Plexxikon, Inc. | Compounds modulating c-fms and/or c-kit activity and uses therefor |
| WO2008094860A2 (en) | 2007-01-30 | 2008-08-07 | Allergan, Inc. | Treating ocular diseases using peroxisome proliferator-activated receptor delta antagonists |
| CN103497185A (zh) | 2007-03-14 | 2014-01-08 | 兰贝克赛实验室有限公司 | 用作磷酸二酯酶抑制剂的吡唑并(3,4-b)吡啶衍生物 |
| EP2170830B1 (en) | 2007-07-17 | 2014-10-15 | Plexxikon, Inc. | 2-FLUORO-BENZENESULFONAMIDE COMPOUNDS AS Raf KINASE MODULATORS |
| GB0715048D0 (en) * | 2007-08-02 | 2007-09-12 | Glaxo Group Ltd | Novel compounds |
| US8158636B2 (en) | 2008-05-19 | 2012-04-17 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| ES2445199T3 (es) | 2008-06-05 | 2014-02-28 | Glaxo Group Limited | Derivados de benzpirazol como inhibidores de PI3-quinasas |
| ES2526966T3 (es) | 2008-06-05 | 2015-01-19 | Glaxo Group Limited | Compuestos novedosos |
| ATE552255T1 (de) | 2008-06-05 | 2012-04-15 | Glaxo Group Ltd | 4-aminoindazole |
| WO2010102958A1 (en) | 2009-03-09 | 2010-09-16 | Glaxo Group Limited | 4-oxadiazol-2 -yl- indazoles as inhibitors of p13 kinases |
| CA2759476C (en) | 2009-04-30 | 2018-10-09 | Julie Nicole Hamblin | Novel compounds |
| KR20120097512A (ko) | 2009-11-18 | 2012-09-04 | 플렉시콘, 인코퍼레이티드 | 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증 |
| KR20120112623A (ko) | 2009-12-23 | 2012-10-11 | 플렉시콘, 인코퍼레이티드 | 키나제 조절을 위한 화합물 및 방법, 및 그에 대한 적응증 |
| RU2012136451A (ru) | 2010-01-28 | 2014-03-10 | Президент Энд Феллоуз Оф Гарвард Колледж | Композиции и способы улучшения активности протеасомы |
| TWI510487B (zh) | 2010-04-21 | 2015-12-01 | Plexxikon Inc | 用於激酶調節的化合物和方法及其適應症 |
| GB201018124D0 (en) | 2010-10-27 | 2010-12-08 | Glaxo Group Ltd | Polymorphs and salts |
| WO2012109075A1 (en) | 2011-02-07 | 2012-08-16 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| JP6208122B2 (ja) | 2011-05-12 | 2017-10-04 | プロテオステイシス セラピューティクス，インコーポレイテッド | プロテオスタシス調節因子 |
| RU2631487C2 (ru) | 2011-05-17 | 2017-09-22 | Плексксикон Инк. | Модуляция киназ и показания к её применению |
| US9358235B2 (en) | 2012-03-19 | 2016-06-07 | Plexxikon Inc. | Kinase modulation, and indications therefor |
| JP6318156B2 (ja) | 2012-09-06 | 2018-04-25 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | キナーゼをモジュレートするための化合物および方法、ならびにその指標 |
| US9163021B2 (en) | 2012-10-04 | 2015-10-20 | Pfizer Limited | Pyrrolo[3,2-c]pyridine tropomyosin-related kinase inhibitors |
| PE20151280A1 (es) | 2012-12-21 | 2015-09-12 | Plexxikon Inc | Compuestos y metodos para la modulacion de quinasas y sus indicaciones |
| US9849135B2 (en) | 2013-01-25 | 2017-12-26 | President And Fellows Of Harvard College | USP14 inhibitors for treating or preventing viral infections |
| NZ630875A (en) | 2013-03-15 | 2017-12-22 | Plexxikon Inc | Heterocyclic compounds and uses thereof |
| US20140303121A1 (en) | 2013-03-15 | 2014-10-09 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| CA2912568A1 (en) | 2013-05-30 | 2014-12-04 | Plexxikon Inc. | Compounds for kinase modulation, and indications therefor |
| WO2015073528A1 (en) | 2013-11-12 | 2015-05-21 | Proteostasis Therapeutics, Inc. | Proteasome activity enhancing compounds |
| WO2015134536A1 (en) | 2014-03-04 | 2015-09-11 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2016044067A1 (en) | 2014-09-15 | 2016-03-24 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| US10160755B2 (en) | 2015-04-08 | 2018-12-25 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2017019804A2 (en) | 2015-07-28 | 2017-02-02 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| CA3129180A1 (en) | 2015-09-21 | 2017-03-30 | Plexxikon Inc. | Heterocyclic compounds and uses thereof |
| US9938273B2 (en) | 2015-12-07 | 2018-04-10 | Plexxikon Inc. | Compounds and methods for kinase modulation, and indications therefor |
| WO2017123826A1 (en) | 2016-01-14 | 2017-07-20 | Beth Israel Deaconess Medical Center, Inc. | Mast-cell modulators and uses thereof |
| JP6921846B6 (ja) | 2016-03-16 | 2021-09-15 | プレキシコン インコーポレーテッドＰｌｅｘｘｉｋｏｎ Ｉｎｃ． | キナーゼ調節およびその適応症のための化合物および方法 |
| TW201819361A (zh) | 2016-09-03 | 2018-06-01 | 印度商托仁特生技有限公司 | 新穎吲唑化合物 |
| TW201815766A (zh) | 2016-09-22 | 2018-05-01 | 美商普雷辛肯公司 | 用於ｉｄｏ及ｔｄｏ調節之化合物及方法以及其適應症 |
| JP7193460B2 (ja) | 2016-12-23 | 2022-12-20 | プレキシコン インコーポレーテッド | Ｃｄｋ８調節およびその適応症のための化合物および方法 |
| WO2018175311A1 (en) | 2017-03-20 | 2018-09-27 | Plexxikon Inc. | Crystalline forms of 4-(1-(1,1-di(pyridin-2-yl)ethyl)-6-(3,5-dimethylisoxazol-4-yl)-1h- pyrrolo[3,2-b]pyridin-3-yl)benzoic acid that inhibits bromodomain |
| US10428067B2 (en) | 2017-06-07 | 2019-10-01 | Plexxikon Inc. | Compounds and methods for kinase modulation |
| KR102615829B1 (ko) | 2017-07-25 | 2023-12-20 | 플렉시콘 인코퍼레이티드 | 키나제를 조정하는 화합물의 제제 |
| AU2018348241B2 (en) | 2017-10-13 | 2023-01-12 | Opna Bio SA | Solid forms of a compound for modulating kinases |
| CN109678784A (zh) * | 2017-10-19 | 2019-04-26 | 天津师范大学 | 硫醚化吲哚类化合物及其制备方法 |
| CA3080197C (en) | 2017-10-27 | 2023-12-19 | Plexxikon Inc. | Formulations of a compound modulating kinases |
| EP3768666A1 (en) | 2018-03-20 | 2021-01-27 | Plexxikon Inc. | Compounds and methods for ido and tdo modulation, and indications therefor |
| CN113993845A (zh) * | 2019-06-17 | 2022-01-28 | 优时比制药有限公司 | 作为治疗cns障碍例如多发性硬化的gpr17调节剂的n-(苯基)-吲哚-3-磺酰胺衍生物和相关化合物 |
| CA3176237A1 (en) | 2020-04-29 | 2021-11-04 | Jack Lin | Synthesis of heterocyclic compounds |
Family Cites Families (18)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US3511841A (en) * | 1967-05-29 | 1970-05-12 | Sterling Drug Inc | 1-((4-,5-,6-,and 7-azaindolyl)-lower-alkyl)- 4-substituted-piperazines |
| US3557142A (en) * | 1968-02-20 | 1971-01-19 | Sterling Drug Inc | 4,5,6,7-tetrahydro-indole-lower-alkanoic acids and esters |
| US5075313A (en) * | 1990-09-13 | 1991-12-24 | Eli Lilly And Company | 3-aryl-4(3H)quinazolinone CCK antagonists and pharmaceutical formulations thereof |
| CA2186499A1 (en) * | 1994-03-30 | 1995-10-12 | Kiyoshi Yoshida | Indole derivative and medicine containing the same |
| ATE333275T1 (de) * | 1998-02-23 | 2006-08-15 | Univ South Alabama | Indole-3-propionsäure, ihre salze und ester als arzneimittel |
| US6329389B1 (en) * | 1998-04-08 | 2001-12-11 | Takeda Chemical Industries, Ltd. | Amine compounds, their production and use |
| US6331537B1 (en) * | 1998-06-03 | 2001-12-18 | Gpi Nil Holdings, Inc. | Carboxylic acids and carboxylic acid isosteres of N-heterocyclic compounds |
| TNSN99224A1 (fr) * | 1998-12-01 | 2005-11-10 | Inst For Pharm Discovery Inc | Methodes de reduction des niveaux de glucose et triglyceride en serum et pour suppression de l'antigenese utilisant les acides la indolealkanoique |
| US6608059B1 (en) * | 2000-06-27 | 2003-08-19 | Smithkline Beecham Corporation | Fatty acid synthase inhibitors |
| BR0212512A (pt) * | 2001-09-14 | 2004-10-26 | Tularik Inc | Composto, composição farmacêutica e métodos para tratar um distúrbio, condição ou doença, elevar os nìveis do colesterol hdl, reduzir os nìveis de triglicerìdeo, tratar diabete, diminuir a resistência à insulina ou diminuir a pressão arterial e modular a ppardelta |
| MXPA04007414A (es) * | 2002-02-01 | 2004-10-11 | Hoffmann La Roche | Indoles sustituidos como agonistas alfa-1. |
| SE0202241D0 (sv) * | 2002-07-17 | 2002-07-17 | Astrazeneca Ab | Novel Compounds |
| CA2495943C (en) * | 2002-08-29 | 2009-07-21 | Merck & Co., Inc. | Indoles having anti-diabetic activity |
| CA2532403A1 (en) * | 2003-07-17 | 2005-02-03 | James Arnold | Ppar active compounds |
| US7348338B2 (en) * | 2003-07-17 | 2008-03-25 | Plexxikon, Inc. | PPAR active compounds |
| US20070232681A1 (en) * | 2003-10-14 | 2007-10-04 | Oxagen Limited | Compounds Having Crth2 Antagonist Activity |
| WO2005056522A2 (en) * | 2003-12-04 | 2005-06-23 | National Health Research Institutes | Indole compounds |
| GB0412914D0 (en) * | 2004-06-10 | 2004-07-14 | Oxagen Ltd | Compounds |
-
2005
- 2005-11-29 US US11/289,781 patent/US20060135540A1/en not_active Abandoned
- 2005-11-29 CA CA002589896A patent/CA2589896A1/en not_active Abandoned
- 2005-11-29 AU AU2005311826A patent/AU2005311826A1/en not_active Abandoned
- 2005-11-29 WO PCT/US2005/043412 patent/WO2006060535A2/en not_active Ceased
- 2005-11-29 EP EP05852598A patent/EP1833787A2/en not_active Withdrawn
- 2005-11-29 JP JP2007543613A patent/JP2008521831A/ja active Pending